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Submit ReviewEPZ 015666
说明： Potent and selective PRMT5 inhibitor
化学名： N-[(2S)-3-(3,4-Dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-6-(3-oxetanylamino)-4-pyrimidinecarboxamide
纯度： ≥98% (HPLC)
生物活性 for EPZ 015666
EPZ 015666 is a potent and selective protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50 = 22 nM, Ki = 5 nM). Displays selectivity for PRMT5 over a panel of 20 other protein methyltransferases. Exhibits dose-dependent antitumor effects in multiple mantle cell lymphoma (MCL) xenograft models. Orally bioavailable.
化合物库 for EPZ 015666
EPZ 015666 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
技术数据 for EPZ 015666
| 分子量 | 383.44 |
| 公式 | C20H25N5O3 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1616391-65-1 |
| PubChem ID | 90241673 |
| InChI Key | ZKXZLIFRWWKZRY-KRWDZBQOSA-N |
| Smiles | O[C@H](CN1CCC2=CC=CC=C2C1)CNC(C3=NC=NC(NC4COC4)=C3)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for EPZ 015666
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 38.34 | 100 | |
| ethanol | 19.17 | 50 |
制备储备液 for EPZ 015666
以下数据基于产品分子量 383.44。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.61 mL | 13.04 mL | 26.08 mL |
| 5 mM | 0.52 mL | 2.61 mL | 5.22 mL |
| 10 mM | 0.26 mL | 1.3 mL | 2.61 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
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产品说明书 for EPZ 015666
参考文献 for EPZ 015666
参考文献是支持产品生物活性的出版物。
Duncan et al (2015) Structure and property guided design in the identification of PRMT5 tool compound EPZ015666. ACS Med.Chem.Lett. 7 162 PMID: 26985292
Chan-Penebre et al (2015) A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models. Nat.Chem.Biol. 11 432 PMID: 25915199
If you know of a relevant reference for EPZ 015666, please let us know.
关键词: EPZ 015666, EPZ 015666 supplier, EPZ015666, GSK3235025, potent, selective, PRMT5, protein, arginine, methytransferase, 5, inhibitors, inhibits, Protein, Arginine, Methyltransferases, 6516, Tocris Bioscience
1 篇 EPZ 015666 的引用文献
引用文献是使用了 Tocris 产品的出版物。 EPZ 015666 的部分引用包括：
Omar et al (2019) Therapeutic Targeting of RNA Splicing Catalysis through Inhibition of Protein Arginine Methylation. Cancer Cell 36 194-209.e9 PMID: 31408619
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.